CN101765597A - 作为磷脂酰肌醇-3-激酶抑制剂的嘧啶衍生物 - Google Patents

作为磷脂酰肌醇-3-激酶抑制剂的嘧啶衍生物 Download PDF

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Publication number
CN101765597A
CN101765597A CN200880019513A CN200880019513A CN101765597A CN 101765597 A CN101765597 A CN 101765597A CN 200880019513 A CN200880019513 A CN 200880019513A CN 200880019513 A CN200880019513 A CN 200880019513A CN 101765597 A CN101765597 A CN 101765597A
Authority
CN
China
Prior art keywords
base
pyrimidine
morpholine
fluoro
indoles
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN200880019513A
Other languages
English (en)
Chinese (zh)
Inventor
P·J·戈德史密斯
T·C·汉科克斯
N·A·佩格
S·J·舒特尔沃思
E·A·德肖瓦
S·普赖斯
J·M·拉奇
E·麦唐纳
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Institute of Cancer Research Royal Cancer Hospital
Original Assignee
F Hoffmann La Roche AG
Institute of Cancer Research Royal Cancer Hospital
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0707088A external-priority patent/GB0707088D0/en
Priority claimed from GB0707611A external-priority patent/GB0707611D0/en
Application filed by F Hoffmann La Roche AG, Institute of Cancer Research Royal Cancer Hospital filed Critical F Hoffmann La Roche AG
Publication of CN101765597A publication Critical patent/CN101765597A/zh
Pending legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Dental Preparations (AREA)
CN200880019513A 2007-04-12 2008-04-14 作为磷脂酰肌醇-3-激酶抑制剂的嘧啶衍生物 Pending CN101765597A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB0707088.1 2007-04-12
GB0707088A GB0707088D0 (en) 2007-04-12 2007-04-12 Pharmaceutical compounds
GB0707611A GB0707611D0 (en) 2007-04-19 2007-04-19 Pharmaceutical compounds
GB0707611.0 2007-04-19
PCT/GB2008/001301 WO2008125839A2 (en) 2007-04-12 2008-04-14 Pyrimidine derivatives as inhibitors of phosphatidylinositol-3-kinase

Publications (1)

Publication Number Publication Date
CN101765597A true CN101765597A (zh) 2010-06-30

Family

ID=39832798

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200880019513A Pending CN101765597A (zh) 2007-04-12 2008-04-14 作为磷脂酰肌醇-3-激酶抑制剂的嘧啶衍生物

Country Status (13)

Country Link
US (1) US20100130496A1 (de)
EP (1) EP2150546B1 (de)
JP (1) JP2010523639A (de)
KR (1) KR20100016433A (de)
CN (1) CN101765597A (de)
AT (1) ATE496045T1 (de)
AU (1) AU2008237721A1 (de)
BR (1) BRPI0810641A2 (de)
CA (1) CA2683624A1 (de)
DE (1) DE602008004650D1 (de)
IL (1) IL201365A0 (de)
MX (1) MX2009010886A (de)
WO (1) WO2008125839A2 (de)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105745194A (zh) * 2013-11-15 2016-07-06 拜耳作物科学股份公司 腈的催化氢化
CN108884046A (zh) * 2016-02-12 2018-11-23 葛兰素史克知识产权开发有限公司 作为激酶活性的抑制剂的化学化合物
CN110914265A (zh) * 2017-05-15 2020-03-24 密歇根大学董事会 作为lsd-1抑制剂的吡咯并[2,3-c]吡啶和相关类似物
CN112047938A (zh) * 2019-06-06 2020-12-08 北京泰德制药股份有限公司 作为atr激酶抑制剂的2,4,6-三取代的嘧啶化合物
CN112703187A (zh) * 2018-06-28 2021-04-23 阿泽克制药公司 作为trk受体的调节剂的4-取代的苯基-1,3,5-三嗪衍生物
CN119841806A (zh) * 2023-10-16 2025-04-18 中国医学科学院药物研究所 多取代的喹唑啉类化合物及其制备方法、用途和药物组合物

Families Citing this family (29)

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BRPI0810646A2 (pt) * 2007-04-12 2014-11-04 Hoffmann La Roche " compostos farmacêuticos ".
EP2318377B1 (de) 2008-07-31 2013-08-21 Genentech, Inc. Pyrimidinverbindungen und -zusammensetzungen sowie verfahren zu ihrer verwendung
CA2733533C (en) 2008-08-25 2013-12-17 Irm Llc Hedgehog pathway modulators
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
WO2010092962A1 (ja) 2009-02-12 2010-08-19 アステラス製薬株式会社 へテロ環誘導体
CN102711766B (zh) 2009-11-12 2014-06-04 霍夫曼-拉罗奇有限公司 N-9-取代的嘌呤化合物、组合物和使用方法
CN102712642B (zh) 2009-11-12 2015-08-12 霍夫曼-拉罗奇有限公司 N-7取代的嘌呤和吡唑并嘧啶化合物、组合物和使用方法
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
US8933024B2 (en) 2010-06-18 2015-01-13 Sanofi Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
EP2604601B1 (de) 2010-08-10 2016-02-24 Astellas Pharma Inc. Heteroring-verbindung
US8877934B2 (en) 2010-09-29 2014-11-04 Intervet Inc. N-heteroaryl compounds
AU2011343712B2 (en) 2010-12-16 2015-09-17 Genentech, Inc. Tricyclic PI3k inhibitor compounds and methods of use
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
JP6117235B2 (ja) 2011-12-15 2017-04-19 ノバルティス アーゲー Ｐｉ３ｋの活性または機能の阻害剤の使用
WO2013144179A1 (en) 2012-03-28 2013-10-03 Intervet International B.V. Heteroaryl compounds with a-cyclic bridging unit
EP2852661A1 (de) 2012-05-23 2015-04-01 F. Hoffmann-La Roche AG Zusammensetzungen und verfahren zur gewinnung und verwendung von endodermalen zellen und leberzellen
WO2014068070A1 (en) 2012-10-31 2014-05-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for preventing antiphospholipid syndrome (aps)
CA2940237C (en) 2014-02-21 2023-03-07 Frost Biologic, Inc. Antimitotic amides for the treatment of cancer and proliferative disorders
WO2016059220A1 (en) 2014-10-16 2016-04-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Tcr-activating agents for use in the treatment of t-all
DK3558944T3 (da) 2016-12-21 2022-05-30 Bayer Cropscience Ag Hydrogenering af et substitueret 2-methylcyanopyridylderivat i nærvær af en raney-cobaltkatalysator
WO2019046316A1 (en) * 2017-08-28 2019-03-07 Acurastem Inc. PIKFYVE KINASE INHIBITORS
EP4069366B1 (de) 2019-12-04 2025-03-19 CHDI Foundation, Inc. Atm-kinasehemmer sowie zusammensetzungen und verfahren zur verwendung davon
CN115515588A (zh) 2020-02-14 2022-12-23 萨克生物研究学院 大环ulk1/2抑制剂
AU2021218739A1 (en) * 2020-02-14 2022-09-22 Salk Institute For Biological Studies Inhibitors of ULK1/2 and methods of using same

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU5261001A (en) * 2000-04-27 2001-11-12 Imperial Cancer Research Technology Ltd Condensed heteroaryl derivatives
ATE527250T1 (de) * 2002-11-21 2011-10-15 Novartis Ag 2,4,6-trisubstituierten pyrimidinen als phosphotidylinositol (pi) 3-kinase inhibitoren und deren verwendung zur behandlung von krebs
CA2527079A1 (en) * 2003-05-29 2005-01-06 Synta Pharmaceuticals, Corp. Heterocyclic compounds for preventing and treating disorders associated with excessive bone loss
EP1745033A4 (de) * 2004-05-08 2009-08-26 Neurogen Corp 4,5-disubstituierte 2-aryl-pyrimidine
WO2006060194A1 (en) * 2004-11-19 2006-06-08 Synta Pharmaceuticals Corp. Pyrimidine compounds and uses thereof
GB0520657D0 (en) * 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105745194A (zh) * 2013-11-15 2016-07-06 拜耳作物科学股份公司 腈的催化氢化
CN105745194B (zh) * 2013-11-15 2018-09-25 拜耳作物科学股份公司 腈的催化氢化
CN108884046A (zh) * 2016-02-12 2018-11-23 葛兰素史克知识产权开发有限公司 作为激酶活性的抑制剂的化学化合物
CN108884046B (zh) * 2016-02-12 2021-11-09 葛兰素史克知识产权开发有限公司 作为激酶活性的抑制剂的化学化合物
CN110914265A (zh) * 2017-05-15 2020-03-24 密歇根大学董事会 作为lsd-1抑制剂的吡咯并[2,3-c]吡啶和相关类似物
CN110914265B (zh) * 2017-05-15 2022-12-23 密歇根大学董事会 作为lsd-1抑制剂的吡咯并[2,3-c]吡啶和相关类似物
CN112703187A (zh) * 2018-06-28 2021-04-23 阿泽克制药公司 作为trk受体的调节剂的4-取代的苯基-1,3,5-三嗪衍生物
CN112047938A (zh) * 2019-06-06 2020-12-08 北京泰德制药股份有限公司 作为atr激酶抑制剂的2,4,6-三取代的嘧啶化合物
WO2020244613A1 (zh) * 2019-06-06 2020-12-10 北京泰德制药股份有限公司 作为atr激酶抑制剂的2，4，6-三取代的嘧啶化合物
TWI778366B (zh) * 2019-06-06 2022-09-21 中國商北京泰德製藥股份有限公司 作為atr激酶抑制劑的2,4,6-三取代的嘧啶化合物
US12544382B2 (en) 2019-06-06 2026-02-10 Beijing Tide Pharmaceutical Co., Ltd. 2, 4, 6-tri-substituted pyrimidine compound as ATR kinase inhibitor
CN119841806A (zh) * 2023-10-16 2025-04-18 中国医学科学院药物研究所 多取代的喹唑啉类化合物及其制备方法、用途和药物组合物

Also Published As

Publication number Publication date
AU2008237721A1 (en) 2008-10-23
BRPI0810641A2 (pt) 2019-09-24
DE602008004650D1 (de) 2011-03-03
EP2150546A2 (de) 2010-02-10
WO2008125839A2 (en) 2008-10-23
MX2009010886A (es) 2009-12-14
ATE496045T1 (de) 2011-02-15
IL201365A0 (en) 2010-05-31
CA2683624A1 (en) 2008-10-23
KR20100016433A (ko) 2010-02-12
US20100130496A1 (en) 2010-05-27
WO2008125839A3 (en) 2008-12-24
JP2010523639A (ja) 2010-07-15
EP2150546B1 (de) 2011-01-19

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Application publication date: 20100630